144689-63-4 Olmesartan Medoxomil

Details:

Olmesartan Medoxomil Usage And Synthesis
Description Olmesartan medoxomil was launched in the US as benicar@, an orally administered treatment for hypertension. This ester prodrug of olmesartan can be synthesized in 8 steps from diaminomaleonitrile by successive reactions with trialkylorthopropanoate to access 2-propyl-imidazole-45dicarbonitrile, conversion of the two nitrile functions to the corresponding ethyl esters, followed by methylmagnesium bromide addition to give the corresponding 4-(1-hydroxyalkyl)imidazole derivative. The latter is alkylated with the trityl-protected biphenyl tetrazole derivative. Finally detritylation and alkaline hydrolysis leads to olmesartan, that is esterified to its corresponding prodrug. Olmesartan, is a new selective and competitive nonpeptide angiotensin II type 1 receptor antagonist and potently inhibits the Ang.ll-induced pressor responses. The drug competitively inhibited binding of [125I1]-All to AT1 receptors in bovine adrenal cortical membranes, but had no effect on binding to AT2 receptors in bovine cerebellar membranes. In comparative clinical studies in patients with essential hypertension, olmesartan reduced sitting cuff diastolic blood pressure significantly more than losartan, valdesartan and ibesartan, while reductions in systolic blood pressure were similar for all treatments. Olmesartan medoxomil was also shown to reduce blood pressure significantly more effectively than losartan and the ACE inhibitor captopril and as effectively as the pbloker atenolol. Olmesartan medoxomil is rapidly and completely bioactivated by ester hydrolysis to its active metabolite, olmesartan, during absorption from the gastrointestinal tract. Olmesartan has an absolute bioavailability of approximatively 26%, a mean elimination half-life of 14 h in patients with hypertension and is not further metabolized. Olmesartan medoxomil is well tolerated, has a side-effect profile similar to that of placebo and unlike ACE inhibitors, the incidence of dry cough is rare. .
Chemical Properties White to off-white crystalline powder
Originator Sanky (Japan)
Uses An angiotensin II receptor antagonist. Used as an anti-hypertensive